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  • Title: Telomerase inhibitors--oligonucleotide phosphoramidates as potential therapeutic agents.
    Author: Gryaznov S, Pongracz K, Matray T, Schultz R, Pruzan R, Aimi J, Chin A, Harley C, Shea-Herbert B, Shay J, Oshima Y, Asai A, Yamashita Y.
    Journal: Nucleosides Nucleotides Nucleic Acids; 2001; 20(4-7):401-10. PubMed ID: 11563055.
    Abstract:
    We have designed, synthesized, and evaluated using physical, chemical and biochemical assays various oligonucleotide N3'-->P5' phosphoramidates, as potential telomerase inhibitors. Among the prepared compounds were 2'-deoxy, 2'-hydroxy, 2'-methoxy, 2'-ribo-fluoro, and 2'-arabino-fluoro oligonucleotide phosphoramidates, as well as novel N3'-->P5' thio-phosphoramidates. The compounds demonstrated sequence specific and dose dependent activity with IC50 values in the sub-nM to pM concentration range.
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